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Compound Detail

CHEMBL2417796

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C#CCN(Cc1cc2c(=O)n(C)c(CN3CCN(C)CC3)nc2cc1Br)c1ccc(C(=O)NCc2cccnc2)cc1

Basic Information

ChEMBL ID CHEMBL2417796
Phase Preclinical
Structure Type MOL
InChI Key IEPROPISBJVPKK-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

628.6
MW (Da)
3.41
ALogP
8
HBA
1
HBD
86.6
PSA (Ų)
0.28
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H34BrN7O2
MW 628.57
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -1.68

Activity Summary

EC50 1 meas. best 9.31
IC50 1 meas. best 9.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nicotinamide phosphoribosyltransferase
CHEMBL1744525
IC50 9.64 9.64 0.2 1
WIL2
CHEMBL612809
EC50 9.31 9.31 0.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Nicotinamide phosphoribosyltransferase IC50 = 0.23 nM 9.64 Inhibition of NAMPT (unknown origin) 23679915
WIL2 EC50 = 0.49 nM 9.31 Cytotoxicity against human W1L2 cells 23679915

Literature References

PubMed DOI Target Context # Activities
23679915 10.1021/jm4001049 WIL2 1
23679915 10.1021/jm4001049 Nicotinamide phosphoribosyltransferase 1

Data from ChEMBL 36 via Core Engine